Abstract: An object of the present invention is to provide a combination drug that has remarkably excellent preventive and/or therapeutic effects on polycystic kidney disease. The present invention provides a drug for preventing and/or treating polycystic kidney disease comprising a combination of tolvaptan or a prodrug thereof with a somatostatin derivative, and a method for treating polycystic kidney disease using this drug.
Abstract: Provided is a crystal of a specific oxazole compound that has specific inhibitory activity against PDE4, and that shows excellent stability. Specifically, provided is a crystal of an oxazole compound represented by formula (5) wherein the crystal has peaks at diffraction angles 2?(°) of 9.6±0.2, 19.1±0.2, and 21.2±0.2 in an X-ray powder diffraction pattern measured using CuK? characteristic X-rays.
Abstract: The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein: n is 1 or 2; X is CH or N; Y is selected from CH and C—F; Z is selected from C—Rz and N; R1 is selected from: -(Alk1)t-Cyc1; wherein t is 0 or 1; Optionally substituted C1-6 acyclic hydrocarbon groups R2 is selected from hydrogen; halogen; and C1-3 hydrocarbon groups optionally substituted with one or more fluorine atoms; R3 is hydrogen or a group L-R7; R4 is selected from hydrogen; methoxy; and optionally substituted C1-3 alkyl; and R4a is selected from hydrogen and a C1-3 alkyl group; wherein Rz, Alk1, Cyc1, L1 and R7 are defined herein; provided that the compound is other than 6-benzyl-3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-{2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
Type:
Grant
Filed:
August 15, 2019
Date of Patent:
May 11, 2021
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Valerio Berdini, Ildiko Maria Buck, James Edward Harvey Day, Charlotte Mary Griffiths-Jones, Thomas Daniel Heightman, Steven Howard, Christopher William Murray, David Norton, Marc O'Reilly, Alison Jo-Anne Woolford, Michael Liam Cooke, David Cousin, Stuart Thomas Onions, Jonathan Martin Shannon, John Paul Watts
Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
Type:
Application
Filed:
December 23, 2020
Publication date:
April 22, 2021
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases.
Abstract: The disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.
Abstract: The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Inventors:
Christopher Norbert JOHNSON, Ildiko Maria BUCK, Gianni CHESSARI, James Edward Harvey DAY, Hideto FUJIWARA, Christopher Charles Frederick HAMLETT, Steven Douglas HISCOCK, Rhian Sara HOLVEY, Steven HOWARD, John Walter LIEBESCHUETZ, Nicholas John PALMER, Jeffrey David ST DENIS, David Geoffrey TWIGG, Andrew James WOODHEAD
Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
Type:
Application
Filed:
April 20, 2018
Publication date:
April 8, 2021
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Michael READER, Nicola Elizabeth WILSHER, Mark Henry SAUNDERS, Paul Anthony BAGULEY, Colin Thomas LINDLEY, Robert Craig MELLING, Bozena Ewa ADAMCZYK, Mirka SCARATI
Abstract: A method for evaluating an efficacy of a chemoradiotherapy against squamous cell carcinoma comprises the following steps (a) to (c): (a) detecting an expression level of at least one gene selected from a SIM2 gene and genes co-expressed with the SIM2 gene in a squamous cell carcinoma specimen isolated from a subject; (b) comparing the expression level detected in the step (a) with a reference expression level of the corresponding gene; and (c) determining that an efficacy of a chemoradiotherapy against squamous cell carcinoma in the subject is high if the expression level in the subject is higher than the reference expression level as a result of the comparison in the step (b).
Type:
Grant
Filed:
September 24, 2015
Date of Patent:
April 6, 2021
Assignees:
NATIONAL CANCER CENTER, KYOTO UNIVERSITY, OTSUKA PHARMACEUTICAL CO., LTD.
Abstract: The present invention provides an externally applied composition capable of enhancing a stimulatory effect of an essential oil on IGF-1 secretion, the composition including (A) essential oil; and (B) at least one member selected from the group consisting of purine substances and salts thereof. Further, the present invention provides an externally applied composition capable of increasing the stratum corneum water content of the skin and maintaining transepidermal water loss at an appropriate level.
Abstract: An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s?1 and having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1,000 s?1, as measured.
Abstract: The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is —C(?O)—NH—, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.
Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
Type:
Application
Filed:
November 16, 2020
Publication date:
March 11, 2021
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
Abstract: An improved process for preparing 2-chloro-4-nitroimidazole derivatives which are useful intermediates in the preparation of an anti-tuberculosis drug is provided. The process may comprise the step of chlorinating nitroimidazoles with a chlorinating agent and an activating agent to give 2-chloro-4-nitroimidazole derivatives.
Type:
Application
Filed:
January 29, 2018
Publication date:
February 25, 2021
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Petr NOVAK, Petr ZAHRADNIK, Jiri TAUCHMAN, Jan KOCI, Antonin STURC
Abstract: Provided is a superior, novel hetrocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
Abstract: The present invention provides a sunscreen composition comprising two or more oil-soluble ultraviolet absorbers and composite silicone particles having an average particle diameter of 10 ?m or less.
Type:
Grant
Filed:
January 25, 2013
Date of Patent:
February 23, 2021
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Masahiko Tanaka, Miyoko Ogihara, Junko Kako
Abstract: The present invention provides a compound represented by the formula (T) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
Type:
Application
Filed:
October 19, 2020
Publication date:
February 4, 2021
Applicant:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
Type:
Grant
Filed:
June 20, 2008
Date of Patent:
February 2, 2021
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
Abstract: This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.