Patents Assigned to Kyoto Pharmaceutical Industries, Ltd.
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Patent number: 6410525Abstract: A carbapenem compound of the formula (I) wherein R1 is a group hydrolyzable in the living body, R2 and R3 are the same or different and each is a lower alkyl, R is a group of the formula (B) or (C) wherein R4 and R5 are the same or different and each is a hydrogen atom or a lower alkyl and R6 is an alkyl having 1 to 10 carbon atoms. The carbapenem compound (I) of the present invention is superior in absorption from the digestive tract upon oral administration and shows sufficient antibacterial property against a broad range of bacteria species. Therefore, the compound is extremely useful for the prophylaxis and treatment of infectious diseases (particularly bacterial infection).Type: GrantFiled: October 31, 2000Date of Patent: June 25, 2002Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventor: Hiroshi Matsui
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Patent number: 6342494Abstract: A carbapenem compound of the formula (I) wherein R1 is a group hydrolyzable in the body, R2 is selected from the group consisting of aryl groups optionally substituted by 1-3 alkyl groups having 1-4 carbon atoms, 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl and 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, R3 and R4 are lower alkyl groups which may be the same or different or instead form a 4- to 6-membered cyclic amino with the adjacent nitrogen selected from the group consisting of azetidinyl, pyrrolidinyl and piperidinyl or a pharmaceutically acceptable salt thereof The carbapenem compound (I) and a pharmaceutically acceptable salt thereof of the present invention show superior absorption from digestive tract by oral administration, and sufficient antibacterial activity against a wide variety of bacterial species. Thus, they are extremely useful as agents for the prophylaxis and treatment of infectious diseases, particularly bacterial infectious diseases.Type: GrantFiled: August 4, 1999Date of Patent: January 29, 2002Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroshi Matsui, Masayasu Kasai
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Patent number: 6262108Abstract: The cromoglycic acid compound of the formula (I) has an antirheumatic action, an antiinflammatory action and an immunomodulating action. This compound is effective for the inhibition of the symptoms of chronic rheumatoid arthritis and is associated with fewer side effects. Therefore, the antirheumatic agent of the present invention can be used beneficially for the treatment of rheumatoid arthritis. In addition, this compound has anti-type I and anti-type IV allergic activities. Therefore, the compound can be used beneficially mainly for the treatment of allergic dermatitis, in which a type IV allergic reaction is involved, such as contact dermatitis, in which a type IV allergic reaction is involved, atopic dermatitis, in which type I and type IV allergic reactions are involved and the like.Type: GrantFiled: July 28, 2000Date of Patent: July 17, 2001Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Shohei Nakamura, Mamoru Kanda, Fumio Fukata
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Patent number: 6200988Abstract: A heterocyclic derivative of the formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.Type: GrantFiled: February 18, 2000Date of Patent: March 13, 2001Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
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Patent number: 6201011Abstract: A therapeutic agent for allergic dermatitis caused by type IV allergic reaction, which contains diethyl L-lysylcromoglycate of the formula: or a nontoxic salt thereof as an active ingredient. This therapeutic agent for allergic dermatitis is effective for the treatment of allergic dermatitis caused by type IV allergic reaction, such as contact dermatitis mainly induced by type IV allergic reaction and atopic dermatitis induced by type I and type IV allergic reactions.Type: GrantFiled: February 26, 1999Date of Patent: March 13, 2001Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Shohei Nakamura, Mamoru Kanda
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Patent number: 6149923Abstract: An antirheumatic agent comprising diethyl L-lysylcromoglycate of the following formula ##STR1## or a nontoxic salt thereof as an active ingredient. This compound has an anti-inflammatory action and immunomodulating action, is absorbed by oral administration to be delivered efficiently to local sites, and is associated with fewer side effects, so that it serves well as an antirheumatic agent that can be administered orally.Type: GrantFiled: December 10, 1998Date of Patent: November 21, 2000Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroaki Shirahase, Akihisa Yoshimi, Fumio Fukata, Hideki Okunishi, Yuta Kobayashi
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Patent number: 6063806Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.Type: GrantFiled: April 3, 1998Date of Patent: May 16, 2000Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
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Patent number: 5538973Abstract: An imidazole derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof is described. A method for producing the compound or its salt, and its pharmaceutical use, particularly as an agent for the prophylaxis and treatment of the diseases induced by thromboxane A.sub.2 or histamine are described. Also, compounds of the formula (II) and (IV) ##STR2## wherein each symbol is as defined in the specification are described. The imidazole derivative and its parmacologically acceptable salt are useful as agents for the prophylaxis and treatment of the diseases induced by thromboxane A.sub.2 or histamine, and the intermediate compounds (II) and (IV) are novel compounds.Type: GrantFiled: February 23, 1995Date of Patent: July 23, 1996Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroshi Matsui, Shoji Kamiya, Hiroaki Shirahase, Shohei Nakamura
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Patent number: 5491171Abstract: A pharmaceutical preparation for rectal or vaginal administration, comprising a prostaglandin compound and an alkali metal salt of a fatty acid having 8 to 12 carbon atoms, and a method for administering a prostaglandin compound, comprising rectally or vaginally administering same in the presence of an alkali metal salt of a fatty acid.According to the present invention, absorption of prostaglandin from rectum or vagina can be enhanced.The prostaglandin can be stabilized in the preparation.Type: GrantFiled: July 27, 1994Date of Patent: February 13, 1996Assignees: Kyoto Pharmaceutical Industries, Ltd., The Green Cross CorporationInventors: Ken-ichi Nishimura, Akihisa Yoshimi, Takayoshi Mori, Nobuharu Kakeya, Masahiro Kikuchi, Nobuo Kondoh, Takeshi Uchida, Koichi Yamanouchi
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Patent number: 5389625Abstract: Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.Type: GrantFiled: June 8, 1992Date of Patent: February 14, 1995Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroyuki Muro, Masayasu Kasai, Satoru Hatano, Ken-ichi Nishimura, Susumu Nishizawa, Nobuharu Kakeya
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Patent number: 4943567Abstract: Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.Type: GrantFiled: May 27, 1988Date of Patent: July 24, 1990Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Susumu Nishizawa, Hiroyuki Muro, Masayasu Kasai, Satoru Hatano, Syouzi Kamiya, Nobuharu Kakeya, Kazuhiko Kitao
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Patent number: 4937242Abstract: 1,4-Dihydropyridine derivatives of the general formula: ##STR1## wherein X.sup.1 and X.sup.2 independently represent hydrogen, fluoromethyl, fluoromethoxy, halogen, cyano, or nitro; R.sup.1 represents a lower alkyl; R.sup.2 represents acyl, alkoxycarbonyl, acylalkyl, an N-alkyl-substituted carbamoylalkyl, alkoxyalkyl, alkoxycarbonylalkyl, acyloxyalkyl, nitratoalkyl, cyanoalkyl, heterocycle-alkyl, haloalkyl, alkenyl, or alkynyl; A represents an alkylene comprising a carbon atom to which 2 alkyls are bonded and having in total at least 5 carbon atoms; m represents the integer 1, 2 or 3; acid addition salts thereof; a method of production thereof; and pharmaceutical compositions containing such compound(s).Such compounds have pharmacological activities, in particular potent and long lasting hypotensive activity, coronary vasodilatation, cerebral vasodilatation, peripheral vasodilatation, renal vasodilatation and platelet aggregation inhibitory activity.Type: GrantFiled: March 8, 1988Date of Patent: June 26, 1990Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Hiroshi Matsui, Fumio Fukata, Takayoshi Mori, Nobuharu Kakeya, Kazuhiko Kitao
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Patent number: 4847286Abstract: Cromoglycic acid derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (for ester bonding) whose amino group may optionally be substituted by at least one lower alkyl group, and R.sup.2 and R.sup.3 each independently is a lower alkyloxy-substituted or an unsubstituted lower alkyl group, an 1-alkanoyloxyalkyl group, an 1-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1,3-dioxol-2-on-4-ylmethyl group; nontoxic salts thereof; and pharmaceutical compositions containing such compounds. Since the compounds have antiallergic activity and are readily absorbable into the blood stream, they are useful as oral antiallergic agents.Type: GrantFiled: March 27, 1987Date of Patent: July 11, 1989Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Satoshi Tamaki, Masaru Kitagawa, Hirokazu Tsuda, Susumu Nishizawa, Nobuhara Kakeya, Kazuhiko Kitao
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Patent number: 4605651Abstract: 1. A cephalosporin derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (bonded by the ester linkage), which may optionally be substituted by one or two lower alkyl groups at the amino group thereof, R.sup.2 is an 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl or 5-methyl-1,3-dioxolen-2-on-4-ylmethyl group, R.sup.3 is a carbamoyloxymethyl group, which may optionally be substituted by one or two lower alkyl groups, or a heterocyclothiomethyl group, which may optionally be substituted by one or more appropriate substituents, and R.sup.4 is a hydrogen atom or a hydroxy group, or its non-toxic salt are found to be useful as orally administrable antibiotics having broad antimicrobial activities against both gram-positive and gram-negative bacteria.Type: GrantFiled: October 11, 1983Date of Patent: August 12, 1986Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Nobuharu Kakeya, Susumu Nishizawa, Satoshi Tamaki, Kazuhiko Kitao