PATENTSCOPE: EN_ALL:nmr AND PA:daiichi

N-PHOSPHONOXYMETHYL PRODRUGS OF HYDROXYALKYL THIADIAZOLE DERIVATIVES (Fri, 21 Sep 2018)
There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. As a result of intensive research, the present inventors have found that N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives represented by general formula (I), a regioisomer, a stereoisomer, or a pharmaceutically acceptable salt thereof possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.
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SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY (Fri, 29 Jun 2018)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
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OXAZEPINE DERIVATIVES HAVING TNAP INHIBITORY ACTIVITY (Fri, 29 Jun 2018)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
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PYRIDINE COMPOUND (Fri, 06 Apr 2018)
The present invention relates to a compound having RET kinase inhibiting action or a pharmaceutically acceptable salt thereof, useful in the treatment of diseases such as cancer. In particular a compound represented by the following general formula (I) as defined herein: (I) or a pharmaceutically acceptable salt thereof.
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HYDROXYALKYL THIADIAZOLE DERIVATIVES (Fri, 07 Apr 2017)
Problem to be solved. There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. Solution to the Problem. As a result of intensive research, the present inventors have found that a compound represented by general formula (I), a stereoisomer, or a pharmaceutically acceptable salt thereof inhibits DNA gyrase GyrB subunit and/or topoisomerase IV ParE subunit, possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.
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PYRIDO-OXAZINONE DERIVATIVES AS TNAP INHIBITORS (Fri, 13 Jan 2017)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) : wherein R1 represents a hydrogen atom, an optionally substituted Cl-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted Cl-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted Cl-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted Cl-6 alkoxy group or the like, X represents -CH=, -C(-R7)=, or -N=, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.
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SYNTHESIS OF 1 H-PYRROLO[2,3-B]PYRIDIN DERIVATIVES THAT MODULATE KINASES (Fri, 11 Nov 2016)
The present disclosure provides processes for the preparation of a compound of formula (I): or a salt thereof, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula (I).
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6-MORPHOLINYL-2-PYRAZOLYL-9H-PURINE DERIVATIVES AND THEIR USE AS PI3K INHIBITORS (Fri, 07 Oct 2016)
The present invention relates to a pyrazole derivative of formula (I), a 5 pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof, stereoisomer thereof or a deuterium form thereof, wherein, n, Y, Ra, R1, R2, R3, R4, R5 and R6 are as defined hereinafter in the specification, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. formula (I) Particularly, the present invention provides a compound of formula (I) as inhibitors of phosphatidylinositol-3-kinase (PI3K), which can be used for treating or preventing inflammatory, autoimmune, orphan and hyperproliferative disease and disorder.
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TRICYCLIC BENZOXABOROLES AS ANTIBACTERIAL AGENTS (Fri, 08 Jan 2016)
The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra- abdominal infections (lAls) or bacteremia.
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ANTI-HER3 ANTIBODY-DRUG CONJUGATE (Fri, 16 Oct 2015)
To provide an antitumor drug having excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER3 antibody via a linker having a structure represented by the formula: -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- or -L1-L2-LP- (the anti-HER3 antibody is connected to the terminal of L1, the antitumor compound is connected to the carbonyl group of -(CH2)n2-C(=O)- moiety or the C terminal of LP, with the nitrogen atom of the amino group at position 1 as a connecting position).
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PYRROLIDINE DERIVATIVES WITH ANTIBACTERIAL PROPERTIES (Fri, 14 Feb 2014)
Provided is a compound of Formula (I) or a salt thereof: Formula (I) wherein R, m, n, R1, R2, Aa-Ac are defined as in the claims and ArI represents a bicyclic heterocyclic group of the following formula: Formula (2) Ar 2 represents a bicyclic heterocyclic group of the formula: [Formula 3] having antibacterial activity.
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HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS (Fri, 30 Nov 2012)
The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.
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1-PHENYLPYRROLE COMPOUNDS (Fri, 16 Apr 2010)
The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases, nephropathy, fibrosis, primary aldosteronism or edema. The compound is of the following general formula (I): wherein R1 represents a C1 -C3 alkyl group; R2 represents a hydroxy -C1 -C4 alkyl group and the like; R3 represents a halogeno group, a halogeno-C1 -C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like,- R5 represents a sulfamoyl group or a C1-C3 alkylsulf onyl group; R6 represents a hydrogen atom, a halogeno group and the like] or an N-oxide, atropisomer of the foregoing, or pharmaceutically acceptable salt of the foregoing.
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ATROPISOMERS OF (HYDROXYALKYL) PYRROLE DERIVATIVES (Fri, 16 Apr 2010)
The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I ) : wherein R1 represents a C1-C3 alkyl group; R2 represents a 2-hydroxy- C4-C6 alkyl group; R3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R4 represents a hydrogen atom, a halogeno group and the like; R5 represents a C1-C3 alkyl group; and R6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.
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METHOD FOR MANUFACTURING NEURAMINIC ACID DERIVATIVES (Fri, 24 Oct 2008)
A method for manufacturing neuraminic acid derivatives is provided, also synthetic intermediates of the neuraminic acid derivatives and methods for their manufacture, and neuraminic acid derivatives having high purity. [Means for solution] A synthetic intermediate compound represented by the formula (7) is provided: [wherein R3 represents alkyl; R4 and R5 each represents H, alkyl, phenyl, or together represent tetramethylene, pentamethylene, oxo].
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FUSED SUBSTITUTED AMINOPYRROLIDINE DERIVATIVE (Fri, 11 Jul 2008)
A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.
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VLA-4 INHIBITOR COMPOUNDS (Fri, 05 Jan 2001)
Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by formula (I). As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.
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DIAGNOSTIC DRUGS (Fri, 11 Jul 1997)
Diagnostic drugs containing as the active ingredient 5-membered cyclic N-oxyl compounds represented by general formula (I) or (II), wherein R represents C1-4 alkyl; and R?1 and R2¿ represent each hydrogen or C¿1-4? alkyl. By administering such a drug to a living body, information on active oxygen and free radicals present in the tissues of the living body can be obtained in the form of biological images such as ESR, NMR, magnetoencephalogram, etc. Thus it is useful as a diagnostic drug for diseases and symptoms in which active oxygen and free radicals seemingly participate, for example, cerebral ischemia, cardiac diseases, digestive diseases, cancer, aging, inflammation and cataract. By administering the drug to normal or sick test animals, active oxygen and free radicals formed in the tissues or organs in a normal or sick state can be externally detected and imaged. Based on these results, it is usable as a detection reagent for examining in which diseases active oxygen and free radicals participate, thus providing useful medical information. Further, the presence of active oxygen or free radicals in a living tissue can be examined and the quantities thereof can be measured by homogenizing a sample taken up from a living body, adding an appropriate buffer and the drug thereto, reacting the mixture for an appropriate period of time and then measuring the signal strength by ESR. Thus these drugs are useful as reagents for detecting active oxygen in samples taken up from living bodies.
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ETHYNYLTHIAZOLE DERIVATIVE (Fri, 25 Oct 1996)
An ethynylthiazole derivative represented by formula (1), wherein R?1 and R2¿ independently represent a hydrogen atom, a halogen atom, an alkyl group which may have a substituent or a cycloalkyl group which may have a substituent, or R?1 and R2¿ may together form a ring; R3 represents a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group which may have a substituent, an alkoxyl group which may have a substituent, a carboxyl group or an alkoxycarbonyl group which may have a substituent; A represents a group -NHCO-, a group -CONH- or a group -NHSO¿2?-; m is an integer of 0 to 3; and G is a group represented by formula (2) or (3), wherein R?4 and R5¿ independently represent a hydrogen atom or an alkyl group which may have a substituent, or R?4 and R5¿ may together form a ring; n is an integer of 0 or 1; and R6 represents a hydroxyl group or an alkoxyl group which may have a substituent, or formula (3), wherein R7 represents a hydrogen atom, a hydroxyl group, a halogen atom, an alkyl group which may have a substituent, an alkoxyl group which may have a substituent, a cyano group, a nitro group, a carboxyl group or an alkoxycarbonyl group which may have a substituent; q is an integer of 0 or 1; and R8 represents a hydroxyl group or an alkoxyl group which may have a substituent; and an allergic disease treating agent which contains the derivative as its active ingredient.
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