Abstract: The present invention relates to a sulfonamide compound of the formula (I):
wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.
Abstract: There is provided a cyclic lipopeptide acylase which is capable of deacylating the acyl side chain of a cyclic lipopeptide compound, e.g. Substance FR901379 or its analog, of the following general formula [I] with effectiveness as well a method of producing a cyclic peptide compound which comprises using the acylase.
[wherein R1 is acyl;
R2 is hydroxy or acyloxy;
R3 is hydrogen or hydroxy;
R4 is hydrogen or hydroxy;
R5 is hydrogen or hydroxysulfonyloxy; and
R6 is hydrogen or carbamoyl.
Abstract: This invention relates to a hematopoietic stem cell proliferating agent comprising IGF-I, a hematopoietic stem cell proliferating agent comprising IGF-I and at least one protein selected from among SCF, M-CSF, and G-CSF, and a method of growing hematopoietic stem cells which comprises culturing hematopoietic stem cells in a medium containing IGF-I and at least one protein selected from the group consisting of SCF and M-CSF.
Abstract: A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1 is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3 is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substituted lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substituted amino; R4 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5 is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10 is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof.
Abstract: The trihydrates of &bgr;-alanine of the formula
Are disclosed. Also method of antogonizing glycoprotein IIb/IIIa activity using these compounds is also disclosed.
Abstract: There is provided a cyclic lipopeptide acylase which is capable of deacylating the acyl side chain of a cyclic lipopeptide compound, e.g. Substance FR901379 or its analog, of the following general formula [I] with effectiveness as well a method of producing a cyclic peptide compound which comprises using the acylase.
[wherein
R1 is acyl;
R2 is hydroxy or acyloxy;
R3 is hydrogen or hydroxy;
R4 is hydrogen or hydroxy;
R5 is hydrogen or hydroxysulfonyloxy; and
R6 is hydrogen or carbamoyl.
Abstract: The use of a medium-chain fatty acid triglyceride as the dispersant in the preparation of a medicinal aerosol composition comprising tricyclic compound (I) dispersed in a liquefied hydrofluoroalkane propellant is described.
When a liquefied hydrofluoroalkane is added to a kneaded premix of the tricyclic compound (I) and a medium-chain fatty acid triglyceride, the active ingredient is evenly dispersed in the liquefied hydrofluoroalkane.
Therefore, by distributing a dispenser first with the kneaded premix and, then, with a liquefied hydrofluoroalkane under cooling or elevated pressure, there can be provided a medicinal aerosol composition an improved uniformity of content of the active ingredient.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
February 25, 2003
Assignee:
Fujisawa Pharmaceutical Co., Ltd.
Inventors:
Saburo Murata, Fumio Shiomojo, Yuji Tokunaga, Takehisa Hata
Abstract: The present invention provides a new bioactive compound of formula (I), which has an antimicrobial activity against pathogenic microorganisms, and a process for production thereof. Also provided are a pharmaceutical composition comprising the compound and pharmaceutically acceptable carrier, a use of the WF002 as a medicament and use of the compound for manufacture of the medicament for treatment of infectious disease.
Abstract: Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.
Abstract: A compound of 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 possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.
Abstract: The invention relates to a vitreous form of the compound, FR 173657, having the structure of formula (I). This vitreous form has good solid stability and is therefore useful for producing and supplying FR 173657 products whose quality is stable enough to be suitable for medicine.
Abstract: Novel anthranilic acid derivatives having an inhibiting activity of cGMP-PDE are represented by the formula I where A is a lower alkylene group: 1
Abstract: This invention provides &bgr;-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a &bgr;-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and/or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.
Abstract: Propanolamine derivatives represented by the following formula (I):
These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
Abstract: This invention relates to a hematopoietic stem cell proliferating agent comprising IGF-I, a hematopoietic stem cell proliferating agent comprising IGF-I and at least one protein selected from among SCF, M-CSF, and G-CSF, and a method of growing hematopoietic stem cells which comprises culturing hematopoietic stem cells in a medium containing IGF-I and at least one protein selected from the group consisting of SCF and M-CSF.
The hematopoietic stem cell proliferating agent of the invention causes hematopoietic stem cells to proliferate in the undifferentiated state whether in vivo or in vitro and can, therefore, be used for amelioration of the cytopenia induced by radiotherapy or chemotherapy using anticancer drugs, prevention of infectious diseases associated with lymphopenia, or in vitro culture for multiplication of hematopoietic stem cells and extrasomatic culture of recombinant stem cells in gene therapy.
Abstract: A compound of formula (I):
wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.
Abstract: The invention provides a composition for improving an action of an immunosuppressant, comprising insulin-like growth factor I or its analog as an active ingredient.
Abstract: The present invention relates to a method for separating a lactone-containing high-molecular weight compound having an alkyl group as its side chain from a lactone-containing high-molecular weight compound having an alkenyl group as its side chain by using a sulfonic acid group-containing cation exchange resin pretreated with silver ions.