Abstract: The present invention provides a novel industrially excellent and ecological process for producing methylcobalamin which is useful as a medicament etc. More specifically, it provides a process for producing methylcobalamin by reducing cyanocobalamin or hydroxocobalamin in the presence of a reducing agent, and then methylating the reductant by adding a water-soluble methylating agent.
Abstract: The present invention provides a compound that has an excellent inhibitory activity on STAT6 activation and is effective against allergic diseases, and a medicinal composition thereof. According to the present invention, disclosed is the compound represented by the General Formula (I) [where R1 and R2 independently represent a C1-6 alkyl group and the like that may have a hydrogen atom or a substituent; R3 represents a C1-6 alkyl group and the like that may have a substituent; R4 and R5 independent represents a hydrogen atom or a C1-6 alkyl group and the like that may have a substituent; R6 represents a hydrogen atom and the like; W represents —SO2—and the like; and X represents a sulphur atom and the like.] or a salt thereof, or a hydrate thereof.
Abstract: A crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2?±0.2°) of 19.1° in a powder X-ray diffraction.
Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
Type:
Application
Filed:
June 30, 2006
Publication date:
April 12, 2007
Applicant:
Eisai Co., Ltd.
Inventors:
Francis Fang, James Foy, Lynn Hawkins, Charles Lemelin, Andre Lescarbeau, Xiang Niu, Kuo-Ming Wu
Abstract: The present invention relates to compounds and methods useful in the prevention or treatment of diseases or conditions associated with Toll-like receptor 2 activation.
Type:
Grant
Filed:
October 25, 2004
Date of Patent:
April 10, 2007
Assignee:
Eisai Co., Ltd.
Inventors:
Jesse Chow, Fabian Gusovksy, Lynn Hawkins, Mark Spyvee
Abstract: Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2?±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.
Abstract: The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.
Type:
Application
Filed:
August 4, 2006
Publication date:
March 29, 2007
Applicant:
Eisai Co., Ltd.
Inventors:
Afzal Khan, Darren Medland, Gurpreet Bhatia
Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1–R7, X1, X2, R, Q, and n are as defined herein.
Type:
Grant
Filed:
March 21, 2003
Date of Patent:
March 20, 2007
Assignee:
Eisai Co., Ltd.
Inventors:
James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
Abstract: The invention provides methods for treating and preventing cystic fibrosis, radiation therapy-induced emesis, chronic ear infections, bruxism, motion sickness, tooth decay due to emesis and other disorders by administering to a patient a therapeutically effective amount of at least one proton pump inhibitor. In other embodiments, the proton pump inhibitor can be administered with one or more cystic fibrosis drugs, motion sickness drugs, antibiotics, NSAIDs, and migraine drugs.
Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
Abstract: Because there is no fundamental treatment for Down's syndrome, and participation in society is the ultimate goal, the present invention provides a remedy and method for treating Down's syndrome that improve congenital delayed psychomotor development, and promote improvement in the performance of daily activities and socialization. The present invention is directed to a therapeutic agent for Down's syndrome that contains an acetylcholinesterase inhibitor, a therapeutic agent for improving mental retardation in Down's syndrome, and an agent for improving daily activities of patients. Specifically, the acetylcholinesterase inhibitor is donepezil hydrochloride. More specifically, the present invention is directed to a therapeutic agent for Down's syndrome, a therapeutic agent for improving mental retardation in Down's syndrome, and an agent for improving daily activities of patients with an IQ of 48 or lower and/or patients aged 36 or younger.
Abstract: A compound represented by the formula: [wherein R1 is methoxy, methylthio, ethyl, etc.; R5 and R6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and two of R40, R41 and R42 are C1-6 alkoxy while the remaining one is methoxymethyl, etc.], a salt thereof, or a hydrate of the foregoing. This compound has excellent antagonism against corticotropin-releasing factor receptor.
Abstract: An EBV strain infecting epithelial cells and a stomach cancer cell line cancerated by EBV are established to clarify the mechanism of canceration of epithelial cells into stomach cancer by EBV and to develop a chemotherapeutic agent for stomach cancer cancerated by EBV. Further, a stomach cancer cell line stably producing EBV-related antigens is established to develop a diagnostic drug for stomach cancer cancerated by EBV. According to the present invention, GTC-4 cell line was established through culture of stomach cancer tissues. GTC-4 produced the EBV strain infecting epithelial cells and simultaneously produced EBV-related antigens stably in the supernatant.
Abstract: The present invention is directed to methods of treating diseases and disorders related to immune responses by administering one or more immunomodulatory compounds. In particular, the invention is directed to methods of stimulating and reducing immune responses, therapeutic and prophylactic treatment of cancer, treating autoimmune conditions, treating allergic reactions and asthma, and preventing ischemic damage and asthma by administering one or more immunomodulatory compounds.
Abstract: A protective agent for neurons of the central nervous system and a prophylactic and/or therapeutic agent for disorders in neurons of the central nervous system is provided, each including a compound represented by donepezil hydrochloride.
Abstract: The invention relates to immunotherapeutic compounds and to methods for stimulating an immune response in a subject individual at risk for developing cancer, diagnosed with a cancer, in treatment for cancer, or in post-therapy recovery from cancer or the compounds of the invention can be administered as a prophylactic to a subject individual to prevent or delay the development of cancer.
Type:
Application
Filed:
April 26, 2006
Publication date:
January 25, 2007
Applicant:
Eisai Co., Ltd.
Inventors:
Daniel Rossignol, Sally Ishizaka, Lynn Hawkins, Scott Fields
Abstract: A system allows for the safe, rapid, efficient recovery of a drug solution from sealed vials. The system is closed so that highly potent compounds can later be recovered and reworked without large investment in further engineering controls. The system includes three main components: a recovery device that holds sealed vials containing a solution, and provides means to access the contents of the vials; a peristaltic pump that pumps solution out of the vials; and a recovery tank that receives the pumped solution.
Type:
Application
Filed:
July 7, 2005
Publication date:
January 18, 2007
Applicant:
Eisai Co., Ltd.
Inventors:
Brad Mann, Eddie Ballance, Allen Grobin
Abstract: The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
Abstract: A ubiquitin-specific protease occurring in the brain and a DNA encoding it, which are useful for research on the molecular mechanism of the neuroplasticity expression and so on.