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2-Cyano-4-fluoropyrrolidine derivative or salt thereof (Fri, 01 Sep 2006)
Patent 537658 Disclosed is a 2-cyano-4-fluoropyrrolidine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof; wherein A is a group of the general formula (II); wherein B represents carbonyl or sulfonyl; R1 represents methyl or ethyl, each of which may be substituted by a group selected from the group selected from the group consisting of ���OH and fluoro; and R2 represents ���H or methyl. Further disclosed is are pharmaceutical compositions containing the compounds of formula (I) and the use of those compounds in the treatment and/or prevention of insulin-dependent diabetes (type 1 diabetes), non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, or obesity. The pharmaceutical compositions are also useful as a dipeptidyl peptidase IV inhibitor.
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Peptide compounds (Sat, 29 Jan 2005)
Patent 527189 Described is a compound of the formula (I) wherein R1 is benzofuranyl substituted by halogen, or styryl substituted by halogen; R2 is substituted hydroxy, substituted mercapto or substituted sulfonyl; and X is or pharmaceutically acceptable salts thereof. The compound (I) 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 NO-mediated diseases in animals.
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Cyclodepsipeptide compound (Thu, 26 Sep 1996)
The invention relates to compounds of the formula wherein A is a benzyl group which has suitable substituent(s), Aa, B and D are each lower alkyl, and C is hydrogen or lower alkyl, or a salt thereof. Its preparation and medicaments are included.
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Depsipeptide derivative, production thereof and use thereof (Wed, 28 Aug 1996)
Disclosed is a group of compounds conforming to the formula below wherein A is a benzyl group which has suitable substituent(s) or phenyl group which may have suitable substituent(s), Aa is benzyl group which may have suitable substituent(s) or phenyl group which may have suitable substituent(s), B and D are each lower alkyl, C is hydrogen or lower alkyl, and a pharmaceutically acceptable salt thereof. The compound or a salt thereof of the present invention has excellent parasiticidal activities as an anthelmintic agent for animals and human bodies.
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METHOD OF MEASURING SOLID NMR (Fri, 17 May 2013)
PROBLEM TO BE SOLVED: To provide a method of measuring solid NMR. SOLUTION: An NMR spectrum of a solid sample is measured by performing spin locking by irradiating a sample with a radio wave from a direction in which magnetism falls after causing the magnetism to fall by applying 90° pulses to the sample for 1H, and observing the magnetism of 1H or observing the magnetism after moving the magnetism of 1H to another isotope. In the present invention, a mixture including a plurality of solid molecular species is used as the sample, and signals caused by molecular species which do not desired to be observed are removed or attenuated. COPYRIGHT: (C)2013,JPO&INPIT
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Pyrrolopyridazine derivatives (Sat, 01 Mar 2008)
Patent 541232 Disclosed are pyrrolopyridazine derivatives of formula (I), their use as a medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-alpha mediated diseases.
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Microorganism producing cyclic compound (Fri, 28 Jan 2011)
A microorganism which produces compounds useful as an antifungal agent, particularly a therapeutic agent for deep-seated mycoses, such as mycotic sinusitis, is provided. The present inventors have conducted intensive studies on naturally-occurring microorganisms as a research for antifungal compounds, and found a fungus Acremonium persicinum which produces cyclic compounds having a potent antifungal activity and useful as a medicament, particularly an antifungal agent, and the present invention was completed.
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CYCLIC COMPOUND AND SALT THEREOF (Thu, 16 Dec 2010)
A compound useful as an antifungal agent, particularly a therapeutic agent for deep-seated mycoses, is provided. A fungus Acremonium persicinum was collected, and cyclic compounds were isolated from culture liquids thereof. The present inventors confirmed that the cyclic compounds or salts thereof have a potent antifungal activity and are useful as medicaments, particularly an antifungal agent, and thus the present invention was completed. The cyclic compound and the salt thereof according to the present invention can be used as an agent for preventing or treating mycoses, particularly deep-seated mycoses.
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CYCLIC COMPOUND AND SALT THEREOF (Fri, 18 Sep 2009)
A compound useful as an antifungal agent, particularly a therapeutic agent for deep-seated mycoses, is provided. A fungus Acremonium persicinum was collected, and cyclic compounds were isolated from culture liquids thereof. The present inventors confirmed that the cyclic compounds or salts thereof have a potent antifungal activity and are useful as medicaments, particularly an antifungal agent, and thus the present invention was completed. The cyclic compound and the salt thereof according to the present invention can be used as an agent for preventing or treating mycoses, particularly deep-seated mycoses.
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Cyclic hexapeptide derivatives (Sat, 27 Mar 2004)
Patent 520808 Polypeptide compounds represented by the general formula (I) are described wherein R1 is hydrogen or acyl group, R2 is hydrogen or acyl group, R3 is lower alkyl which has one or more hydroxy or protected hydroxy, R4 is hydrogen or hydroxy, R5 is hydrogen, hydroxy, lower alkoxy or hydroxysulfonyloxy, and R6 is hydroxy or acyloxy, or a salt thereof, which has antimicrobial activities (especially, antifungal activities), inhibitory activity on �� -1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases including Pneumocystis carinii infection (e.g.Pneumocystis carinii pneumonia) in a human being or animal.
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Novel salt of quinuclidine derivative (Fri, 14 Sep 2007)
An acid addition salt formed from (-)-(1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline -2-carboxylic acid (3R)-quinuclidin-3-yl ester and an acid selected from the group consisting of (-)-(2S,3S)-tartaric acid, (+)-(2S,3S)-di-o-benzoyltartaric acid, (+)-(2S,3S)-di-o-(4-methylbenzoyl)tartaric acid, (-)-L-phenylalanine, benzenesulfonic acid, cyclohexanesulfamic acid, hydrobromic acid, naphthalene-2-sulfonic acid, sebacic acid, (+)-camphor-10-sulfonic acid, p-toluenesulfonic acid, ethanesulfonic acid, methanesulfonic acid and methyl phosphate. This salt does not show hygroscopicity in such a level that is not desirable for use as a pharmaceutical agent or an active ingredient of a pharmaceutical agent, and therefore is an extremely useful compound for use as a pharmaceutical agent or an active ingredient of a pharmaceutical agent.
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OXADIAZOLIDINEDIONE COMPOUND (Fri, 01 Jul 2011)
Patent 584811 The disclosure relates to oxadiazolidinedione compounds of formula (I) which are useful as a pharmaceutical agent, particularly as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus, wherein the variables shown in the formula are as defined in the specification.
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Immunosuppressive polypeptides and nucleic acids (Fri, 04 May 2012)
The invention provides immunosuppressive polypeptides and nucleic acids encoding such polypeptides. In one aspect, the invention provides mutant CTLA-4 polypeptides and nucleic acids encoding mutant CTLA-4 polypeptides. Compositions and methods for utilizing such polypeptides and nucleic acids are also provided.
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REMEDY FOR OVERACTIVE BLADDER COMPRISING ACETIC ACID ANILIDE DERIVATIVE AS THE ACTIVE INGREDIENT (Mon, 06 Feb 2006)

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Piperazine derivative (Fri, 10 Feb 2017)
[Problem] To provide a compound that can be used as an MC4 receptor agonist. [Solution] The inventors studied MC4 receptor agonists, confirmed that a piperazine derivative has an action, and perfected the present invention. Specifically, this piperazine derivative has an MC4 receptor agonist action and can be used as an agent for the prevention and/or treatment of bladder and urinary tract diseases, especially underactive bladder, hypotonic bladder, noncontracting bladder, detrusor muscle hypoactivity, neurogenic bladder, urethral relaxation failure, detrusor-external sphincter incoordination, and dysuria in benign prostatic hyperplasia.
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Propane-1,3-dione derivatives (Fri, 05 Oct 2001)
Medicinal compositions, in particular, GnRH receptor antagonists comprising propane-1,3-dione derivatives represented by the following general formula (1) as the active ingredient; and novel propane-1,3-dione derivatives having a GnRH antagonism: general formula (1).
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Aminoalcohol derivatives (Fri, 02 Jun 2006)
This invention relates to new aminoalcohol derivatives and salts thereof which are beta-3 P3% adrenergic receptor and useful as a medicament.
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PYRROLIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE THEM (Mon, 17 Feb 1992)

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BENZAZEPINE COMPOUND (Thu, 17 Jan 2013)
[Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
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Carboxylic acid derivative (Fri, 26 Jun 2009)
[PROBLEMS] To provide a compound which is usable as a drug, in particular, an insulin secretagogue or a preventive or remedy for a disease in which GPR40 participates such as diabetes or the like. [MEANS FOR SOLVING PROBLEMS] It is found out that a novel carboxylic acid derivative, which is characterized in that a carboxylic acid is bonded via two atoms to a 6-membered monocyclic aromatic ring and this aromatic ring is further bonded via a linker to a nitrogen-containing bicyclic ring, or its salt has an excellent GPR40 agonist activity. Because of showing excellent effects of promoting insulin secretion and lowering blood glucose level, this carboxylic acid derivative is useful as an insulin secretagogue or a preventive or remedy for diabetes.
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